Michel Bouvier
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View article: The impact of secondary site interactions on the binding specificity of bitopic dopamine D2/D3 receptor ligands
The impact of secondary site interactions on the binding specificity of bitopic dopamine D2/D3 receptor ligands Open
Dysfunction of dopamine receptors and interruption of normal dopaminergic signaling have been linked to severe neuropsychiatric diseases such as schizophrenia, Parkinson's disease and depression. Although these receptors are among the most…
View article: MRAP2 modifies the signaling and oligomerization state of the melanocortin-4 receptor
MRAP2 modifies the signaling and oligomerization state of the melanocortin-4 receptor Open
View article: Decoding ADGRE5: How Proteolytic Cleavage and Mechanical Forces Unleash Cellular Signals
Decoding ADGRE5: How Proteolytic Cleavage and Mechanical Forces Unleash Cellular Signals Open
The adhesion G protein-coupled receptor ADGRE5/CD97 is upregulated in many cancers, representing a potential drug target in oncology/immuno-oncology. Yet, ADGRE5′s activation and signaling mechanisms remain poorly understood. Here, we used…
View article: Intracrine FFA4 signaling controls lipolysis at lipid droplets
Intracrine FFA4 signaling controls lipolysis at lipid droplets Open
G-protein-coupled receptors (GPCRs) can signal from intracellular compartments but the occurrence and relevance of this phenomenon for metabolite-sensing GPCRs is largely unknown. Here, we investigate free fatty acid receptor 4 (FFA4), a m…
View article: Multiple intramolecular triggers converge to preferential G protein coupling in the CB2R
Multiple intramolecular triggers converge to preferential G protein coupling in the CB2R Open
G protein-coupled receptors (GPCRs) are important therapeutic drug targets for a wide range of diseases. Upon activation, GPCRs can initiate several signaling pathways, each with unique therapeutic implications. Therefore, understanding ho…
View article: Gα<sub>s</sub>‐specific structural elements attenuate interactions with regulator of G protein signaling (<scp>RGS</scp>) proteins
Gα<sub>s</sub>‐specific structural elements attenuate interactions with regulator of G protein signaling (<span>RGS</span>) proteins Open
Heterotrimeric (αβγ) G proteins are molecular switches that are activated by G protein‐coupled receptors (GPCRs) and regulate numerous intracellular signaling cascades. Most active Gα subunits are inactivated by regulators of G protein sig…
View article: Profiling of HCAR1 signaling reveals Gα<sub>i/o</sub>and Gα<sub>s</sub>activation without β-arrestin recruitment and the discovery of an allosteric agonist
Profiling of HCAR1 signaling reveals Gα<sub>i/o</sub>and Gα<sub>s</sub>activation without β-arrestin recruitment and the discovery of an allosteric agonist Open
Lactate was long considered a byproduct of glycolysis and associated with various harmful effects. However, the role of lactate was expanded with the finding that it also can act as a signaling molecule through the G protein–coupled recept…
View article: Torsade de Pointes: How Much Do Psychotropics Really Contribute?
Torsade de Pointes: How Much Do Psychotropics Really Contribute? Open
Introduction Based on potential risk of torsade de pointes (TdeP; a rare arrhythmia), regulatory agencies have issue warning for two specific antidepressants. This has translated in clinic as a class effect in that every antidepressant mon…
View article: Author Correction: Systematic protein-protein interaction mapping for clinically relevant human GPCRs
Author Correction: Systematic protein-protein interaction mapping for clinically relevant human GPCRs Open
View article: The cell adhesion molecule CD44 acts as a modulator of 5-HT7 receptor functions
The cell adhesion molecule CD44 acts as a modulator of 5-HT7 receptor functions Open
View article: G protein selectivity profile of GPR56/ADGRG1 and its effect on downstream effectors
G protein selectivity profile of GPR56/ADGRG1 and its effect on downstream effectors Open
GPR56, an adhesion G-protein coupled receptor (aGPCRs) with constitutive and ligand-promoted activity, is involved in many physiological and pathological processes. Whether the receptor’s constitutive or ligand-promoted activation occur th…
View article: G protein selectivity profile of GPR56/ADGRG1 and its effect on downstream effectors
G protein selectivity profile of GPR56/ADGRG1 and its effect on downstream effectors Open
View article: Comprehensive Analysis of Kisspeptin Signaling: Effects on Cellular Dynamics in Cervical Cancer
Comprehensive Analysis of Kisspeptin Signaling: Effects on Cellular Dynamics in Cervical Cancer Open
Kisspeptin, a key neuropeptide derived from the KISS1R gene, is renowned for its critical role in regulating the hypothalamic–pituitary–gonadal axis and reproductive hormone secretion. Beyond its primary function in reproductive biology, e…
View article: Gα<sub>s</sub>-specific structural elements attenuate interactions with RGS proteins
Gα<sub>s</sub>-specific structural elements attenuate interactions with RGS proteins Open
Heterotrimeric (αβγ) G proteins are molecular switches that are activated by G protein-coupled receptors (GPCRs) and regulate numerous intracellular signaling cascades. Most active Gα subunits are inactivated by Regulators of G protein Sig…
View article: Role of the V2R–βarrestin–Gβγ complex in promoting G protein translocation to endosomes
Role of the V2R–βarrestin–Gβγ complex in promoting G protein translocation to endosomes Open
View article: Structure-based discovery of nonopioid analgesics acting through the α2A-adrenergic receptor
Structure-based discovery of nonopioid analgesics acting through the α2A-adrenergic receptor Open
Because nonopioid analgesics are much sought after, we computationally docked more than 301 million virtual molecules against a validated pain target, the α2A-adrenergic receptor (α2AAR), seeking new α2AAR agonists chemotypes that lack the…
View article: G protein-specific mechanisms in the serotonin 5-HT2A receptor regulate psychosis-related effects and memory deficits
G protein-specific mechanisms in the serotonin 5-HT2A receptor regulate psychosis-related effects and memory deficits Open
G protein-coupled receptors (GPCRs) are sophisticated signaling machines able to simultaneously elicit multiple intracellular signaling pathways upon activation. Complete (in)activation of all pathways can be counterproductive for specific…
View article: Comprehensive Analysis of Kisspeptin Signaling: Effects on Cellular Dynamics in Cervical Cancer
Comprehensive Analysis of Kisspeptin Signaling: Effects on Cellular Dynamics in Cervical Cancer Open
Kisspeptin, a key neuropeptide derived from the KISS1 gene, is renowned for its critical role in regulating the hypothalamic-pituitary-gonadal axis and reproductive hormone secretion. Beyond its primary function in reproductive biology, em…
View article: Community guidelines for GPCR ligand bias: IUPHAR review 32
Community guidelines for GPCR ligand bias: IUPHAR review 32 Open
GPCRs modulate a plethora of physiological processes and mediate the effects of one-third of FDA-approved drugs. Depending on which ligand activates a receptor, it can engage different intracellular transducers. This ‘biased signalling’ pa…
View article: Professor Philippe Crine: a hero for children with hypophosphatasia
Professor Philippe Crine: a hero for children with hypophosphatasia Open
View article: MRAP2 modifies the signaling and oligomerization state of the melanocortin-4 receptor
MRAP2 modifies the signaling and oligomerization state of the melanocortin-4 receptor Open
The melanocortin-4 receptor (MC4R) is a G protein-coupled receptor (GPCR) and a key regulator of appetite and metabolism. It can interact with the melanocortin-receptor accessory protein 2 (MRAP2), a single transmembrane helix protein know…
View article: Pharmacological fingerprint of antipsychotic drugs at the serotonin 5-HT2A receptor
Pharmacological fingerprint of antipsychotic drugs at the serotonin 5-HT2A receptor Open
View article: EGFR signaling and pharmacology in oncology revealed with innovative BRET-based biosensors
EGFR signaling and pharmacology in oncology revealed with innovative BRET-based biosensors Open
View article: Multiple triggers converge to preferential effector coupling in the CB2R through a complex allosteric communication network
Multiple triggers converge to preferential effector coupling in the CB2R through a complex allosteric communication network Open
G protein-coupled receptors are important therapeutic drug targets for a wide range of diseases. Their ability to preferentially engage specific signaling pathways over others can be exploited to design drugs that target only disease-assoc…
View article: Molecular determinants of ligand efficacy and potency in GPCR signaling
Molecular determinants of ligand efficacy and potency in GPCR signaling Open
Heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptors (GPCRs) bind to extracellular ligands and drugs and modulate intracellular responses through conformational changes. Despite their importance as drug targets, …
View article: Quelle légitimité de l’impôt? Quelle légitimité de l’Etat fiscal? Quel nouveau modèle fiscal pour quel nouvel Etat?
Quelle légitimité de l’impôt? Quelle légitimité de l’Etat fiscal? Quel nouveau modèle fiscal pour quel nouvel Etat? Open
The foundations of taxation are seriously threatened by globalization combined with the digital revolution and the multiplicity of challenges that States have to face. This is why there is an urgent need to debate the relevance and future …
View article: How carvedilol does not activate β2-adrenoceptors
How carvedilol does not activate β2-adrenoceptors Open
View article: GLP-1R signaling neighborhoods associate with the susceptibility to adverse drug reactions of incretin mimetics
GLP-1R signaling neighborhoods associate with the susceptibility to adverse drug reactions of incretin mimetics Open
G protein-coupled receptors are important drug targets that engage and activate signaling transducers in multiple cellular compartments. Delineating therapeutic signaling from signaling associated with adverse events is an important step t…
View article: Gαs is dispensable for β-arrestin coupling but dictates GRK selectivity and is predominant for gene expression regulation by β2-adrenergic receptor
Gαs is dispensable for β-arrestin coupling but dictates GRK selectivity and is predominant for gene expression regulation by β2-adrenergic receptor Open
β-arrestins play a key role in G protein-coupled receptor (GPCR) internalization, trafficking, and signaling. Whether β-arrestins act independently of G protein-mediated signaling has not been fully elucidated. Studies using genome-editing…
View article: Efficacy and Safety of Magnetic Seed Pre-Operative Non-Palpable Breast Lesion Localization: a series of 37 consecutive cases
Efficacy and Safety of Magnetic Seed Pre-Operative Non-Palpable Breast Lesion Localization: a series of 37 consecutive cases Open
Context 40% of breast surgery patients have a lesion that requires preoperative localization, a process that demands close cooperation between radiological and surgical team. Magnetic seed localization is a new tracking technique which doe…